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The photodynamic activity of 131-[2'-(2-pyridyl)ethylamine] chlorin e6 photosensitizer in human esophageal cancer.
Srdanovic, Sonja; Gao, Ying-Hua; Chen, Dan-Ye; Yan, Yi-Jia; Margetic, Davor; Chen, Zhi-Long.
  • Srdanovic S; Division of Organic Chemistry and Biochemistry, Ruder Boskovic Institute, Bijenicka c. 54, 10000, Croatia.
  • Gao YH; Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
  • Chen DY; Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
  • Yan YJ; Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China.
  • Margetic D; Division of Organic Chemistry and Biochemistry, Ruder Boskovic Institute, Bijenicka c. 54, 10000, Croatia. Electronic address: margetid@irb.hr.
  • Chen ZL; Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai 201620, China. Electronic address: zlchen1967@qq.com.
Bioorg Med Chem Lett ; 28(10): 1785-1791, 2018 06 01.
Article en En | MEDLINE | ID: mdl-29673979
ABSTRACT
A novel 131-pyridine substituted chlorin e6 derivative (Chlorin A) was synthesized. It has characteristic long wavelength absorption at 664 nm and the emission wavelength at 667 nm. The generation rate of singlet oxygen of this compound is higher than Temoporfin. In vitro, Chlorin A showed higher phototoxicity against the human esophageal cancer cells than Temoporfin while with lower dark-toxicity. Its accumulation effect in mitochondria, lysosomes and endoplasmic reticulum was traced in subcellular localization tests. In flow cytometry obvious apoptosis cells were observed after 2 h irradiation. Significant in vivo photodynamic anti-tumor efficacy was also exhibited on mice bearing esophageal cancer. So Chlorin A could be suggested as a promising anti-tumor drug candidate in photodynamic therapy.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Fotoquimioterapia / Porfirinas / Piridinas / Neoplasias Esofágicas / Fármacos Fotosensibilizantes / Antineoplásicos Límite: Animals / Humans Idioma: En Año: 2018 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Fotoquimioterapia / Porfirinas / Piridinas / Neoplasias Esofágicas / Fármacos Fotosensibilizantes / Antineoplásicos Límite: Animals / Humans Idioma: En Año: 2018 Tipo del documento: Article